This invention relates to compounds that are mammalian metabolites of (xe2x88x92)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol. The compounds of the invention are useful as standards in analytical assays and as therapeutic agents.
Pharmacologically, (xe2x88x92)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol (PPTN) is an estrogen agonist/antagonist that is disclosed in U.S. Pat. No. 5,552,412. An xe2x80x9cestrogen agonist/antagonistxe2x80x9d is compound that affects some of the same receptors that estrogen does, but not necessarily all, and in some instances, it antagonises or blocks estrogen. It is also known as a xe2x80x9cselective estrogen receptor modulatorxe2x80x9d (SERM). Estrogen agonists/antagonists may also be referred to as antiestrogens although they have some estrogenic activity at some estrogen receptors. Estrogen agonists/antagonists are therefore not what are commonly referred to as xe2x80x9cpure antiestrogensxe2x80x9d. Antiestrogens that can also act as agonists are referred to as Type I antiestrogens. Type I antiestrogens activate the estrogen receptor to bind tightly in the nucleus for a prolonged time but with impaired receptor replenishment (Clark, et al., Steroids 1973;22:707; Capony, et al., Mol Cell Endocrinol, 1975;3:233).
The compounds of the present invention are metabolites of PPTN and are believed to possess significant pharmacological activities similar or identical to those possessed by the parent compound; PPTN.